| 靶标 | GluN2B, Glutamate receptor ionotropic, NMDA 2B, GRIN2B, NMDAR2B, NR2B, Glutamate [NMDA] receptor subunit epsilon-2, N-methyl-D-aspartate receptor subunit 3, N-methyl D-aspartate receptor subtype 2B, hNR3, NR3 |
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| 背景 | Glutamate receptor ionotropic, NMDA 2B (GRIN2B) is a ~166 kDa protein. Component of N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with high calcium permeability and voltage-dependent block by Mg(2+). Participates in synaptic plasticity for learning and memory formation by contributing to the long-term depression (LTD) of hippocampus membrane currents. Channel activation requires binding of the neurotransmitter L-glutamate to the GluN2 subunit, glycine or D-serine binding to the GluN1 subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+). NMDARs mediate simultaneously the potassium efflux and the influx of calcium and sodium. Each GluN2 subunit confers differential attributes to channel properties, including activation, deactivation and desensitization kinetics, pH sensitivity, Ca2(+) permeability, and binding to allosteric modulators. 1. Lemke, JR. et al. (2014) Annals of neurology 75, 147-54. PMID: 242728272. Adams, DR. et al. (2014) Molecular genetics and metabolism 113, 161-70. PMID: 248639704. Volgraf, M. et al. (2016) Journal of medicinal chemistry 59, 2760-79. PMID: 269197615. Swanger, SA. et al. (2016) American journal of human genetics 99, 1261-1280. PMID: 278398716. Ogden, KK. et al. (2017) PLoS genetics 13, e1006536. PMID: 280954207. Chen, W. et al. (2017) Molecular pharmacology 91, 317-330. PMID: 281268518. Xu, Y. et al. (2024) Cellular and molecular life sciences : CMLS 81, 153. PMID: 385388659. Hess, SD. et al. (1996) The Journal of pharmacology and experimental therapeutics 278, 808-16. PMID: 8768735 |
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